Our overall objectives, as outlined in the original proposal, are to develop simple and efficient methods for preparing new site-specific antitumor agents. Our strategy is to combine the favorable transport properties of known drugs, such as steroids, or biological molecules with the subtle alkylating power of alpha-methylene lactones, alpha-hydroxymethyl- and alpha-epoxy-acrylates and acrolein derivatives. We hope to combine the bis-alkylating ability of alpha-methylene carbonyl compounds and allylic systems with various carbocyclic and heterocyclic skeletons. In an effort to temper the chemical reactivity of many alkylating agents, we plan to incorporate biological appendages to the reactive functionality and in some cases exercise a pro-drug approach.